다중혈관 관상동맥 환자에서 y-문합을 이용하여 양쪽 내흉동맥만을 사용한 우회술의 조기 성적

抗原变异可使得多种致病微生物易于逃避宿主免疫应答。表达在感染红细胞表面的恶性疟原虫红细胞表面蛋白1（PfPMP1）与感染红细胞、内皮细胞、树突状细胞以及胎盘的单个或多个受体作用，在黏附及免疫逃避中起关键的作用。每个单倍体基因组var基因家族编码约60种成员，通过启动转录不同的var基因变异体为抗原变异提供了分子基础。

疟原虫var基因转换速率变化导致抗原变异[英]／Paul H, Robert P, Christodoulou Z, et al//Proc Natl Acad Sci U S A

Examination of nature's favorite molecules reveals a striking preference for making carbon-heteroatom bonds over carbon-carbon bonds-surely no surprise given that carbon dioxide is nature's starting material and that most reactions are performed in water. Nucleic acids, proteins, and polysaccharides are condensation polymers of small subunits stitched together by carbon-heteroatom bonds. Even the 35 or so building blocks from which these crucial molecules are made each contain, at most, six contiguous C-C bonds, except for the three aromatic amino acids. Taking our cue from nature's approach, we address here the development of a set of powerful, highly reliable, and selective reactions for the rapid synthesis of useful new compounds and combinatorial libraries through heteroatom links (C-X-C), an approach we call "click chemistry". Click chemistry is at once defined, enabled, and constrained by a handful of nearly perfect "spring-loaded" reactions. The stringent criteria for a process to earn click chemistry status are described along with examples of the molecular frameworks that are easily made using this spartan, but powerful, synthetic strategy.

https://www.onlinelibrary.wiley.com/doi/pdf/10.1002/1521-3773%2820010601%2940%3A11%3C2004%3A%3AAID-ANIE2004%3E3.0.CO%3B2-5

Click Chemistry: Diverse Chemical Function from a Few Good Reactions.

https://pubs.rsc.org/en/content/articlepdf/2019/NP/C8NP00092A

Marine natural products.

CA : A Cancer Journal for Clinicians

Microwave irradiation promotes the rapid O,N-acylation–cyclodehydration cascade reaction of oximes and acid chlorides to give oxazoles.

Microwave‐Promoted Oxazole Synthesis: Cyclocondensation Cascade of Oximes and Acyl Chlorides.

Synthesis of the Antitumor Antibiotic LL-C10037α.

A novel hemigramicidin-tempo conjugate has anti-inflammatory effects in vitro and in vivo.: 30

660 Cdc25 dual specificity phosphatases are overexpressed in many human tumors and have oncogenic properties. Although several quinone inhibitors of Cdc25 phosphatase have been identified, their selectivity and cellular mechanisms of action have not been fully established. We synthesized and evaluated five novel quinolinedione congeners of a previously reported Cdc25 inhibitor, 6-chloro-7-(2-morpholin-4-yl-ethylamino)-quinoline-5,8-dione (DA3003-1 or NSC 663284). All five quinolinediones inhibited Cdc25A, B and C. The dehalogenated and minimal structure, JUN1111, was a more selective in vitro inhibitor of Cdc25 phosphatases compared with DA3003-1. Like DA3003-1, JUN1111 caused cell cycle arrest and directly inhibited etopically expressed Cdc25B activity in transfected cells. In vitro Cdc25B inhibition by these compounds was sensitive to dithiothreitol concentration, pH, and the presence of glutathione and catalase, suggesting that oxidation was a mechanism for irreversible Cdc25B inactivation. Mass spectrometric analysis showed that the catalytic cysteine of Cdc25B was indeed irreversibly oxidized to its sulfonic acid (SO 3 ) form upon treatment with DA3003-1. DA3003-1 and JUN1111 were also shown to rapidly generate reactive oxygen species in cells, further supporting enzyme inhibition by oxidation. We propose that these quinolinediones regulate the phosphatase activity of Cdc25 through selective and irreversible oxidation at the active site cysteine.

Redox regulation of Cdc25B by novel cell active quinolinediones

A direct oxazoline→thiazoline conversion can be realized by thiolysis of oxazolines with H2S in methanol/triethylamine, followed by cyclodehydration with Burgess reagent. This protocol is high-yielding, chemoselective, and essentially free of racemization for C(5)-unsubstituted and trans-4,5-disubstituted peptide oxazolines. Thioamide intermediates are obtained regioselectively, thus the thiolysis of oxazolines offers an alternative to the thiation of peptides with Lawesson's reagent.

Peter Wipf

Papers

Microwave‐Promoted Oxazole Synthesis: Cyclocondensation Cascade of Oximes and Acyl Chlorides.

Synthesis of the Antitumor Antibiotic LL-C10037α.

A novel hemigramicidin-tempo conjugate has anti-inflammatory effects in vitro and in vivo.: 30

Redox regulation of Cdc25B by novel cell active quinolinediones

Thiolysis of Oxazolines: A New, Selective Method for the Direct Conversion of Peptide Oxazolines into Thiazolines.